主权项 |
1. A compound having Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein: R1 is selected from
(a) hydrogen,(b) —C(═O)NHRa, wherein Ra is alkyl or substituted alkyl (e.g., C1-C6 alkyl), or aryl or substituted aryl (e.g., CH2C6H5),(c) —C(═O)ORa, wherein Ra is hydrogen, alkyl or substituted alkyl (e.g., C1-C6 alkyl) aryl or substituted aryl (e.g., CH2C6H5), or(d) —CH2X, wherein X is a halogen (e.g., fluoro, chloro, bromo, iodo); R3 is selected from
(a) hydrogen, or(b) C1-C4 alkyl optionally substituted with a carboxylic acid, carboxylate, or carboxylate C1-C8 ester group (—CO2H, —CO2-, —C(═O)OC1-C8), an amide optionally substituted with an alkylheteroaryl group, or a heteroaryl group; Z is an acyl group selected from
(a) or(b) wherein Y is hydrogen or C1-C4 alkyl; R4 is selected from
(i) hydrogen,(ii) C1-C12 alkyl,(iii) C3-C6 cycloalkyl,(iv) C6-C10 aryl,(v) heterocyclyl,(vi) C3-C10 heteroaryl,(vii) aralkyl, and R5 is —C(═O)—R10, wherein R10 is selected from
(i) C1-C12 alkyl optionally substituted with C6-C10 aryl, C1-C10 heteroaryl, amino, or carboxylic acid,(ii) C1-C10 heteroalkyl optionally substituted with C1-C6 alkyl, carboxylic acid, or heterocyclyl,(iii) C3-C6 cycloalkyl optionally substituted with C1-C6 alkyl, optionally substituted C6-C10 aryl, optionally substituted C3-C10 heteroaryl, amino, or carboxylic acid,(iv) C6-C10 aryl optionally substituted with C1-C6 alkyl, optionally substituted C6-C10 aryl, optionally substituted C3-C10 heteroaryl, amino, or carboxylic acid,(v) heterocyclyl,(vi) C3-C10 heteroaryl,(vii) aralkyl, or(viii) heteroalkylaryl; and is selected from whereinR2a and R2b are independently selected from hydrogen and C1-C3 alkyl, andR2c at each occurrence is independently selected from
(a) hydrogen,(b) halogen,(c) C1-C6 alkyl,(d) —XR11, wherein X is selected from O, C(═O), S, S═O, or S(═O)2,(e) —C(═O)N(R12)(R13),(f) —N(R11)(R12)(R13),(g) —N—C(═O)—R11, or(h) —N—C(═O)O—R11,wherein R11, R12, and R13 are independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 heteroalkyl, C2-C6 alkenyl, C6-C10 aryl, aralkyl, and C3-C10 heteroaryl; andm is 1, 2, 3, or 4; whereinR2a and R2b are independently selected from hydrogen and C1-C3 alkyl, andR2c at each occurrence is independently selected from
(a) hydrogen,(b) halogen,(c) C1-C6 alkyl,(d) —XR11, wherein X is selected from O, C(═O), S, S═O, or S(═O)2,(e) —C(═O)N(R12)(R13),(f) —N(R11)(R12)(R13),(g) —N—C(═O)—R11, or(h) —N—C(═O)O—R11,wherein R11, R12, and R13 are independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 heteroalkyl, C2-C6 alkenyl, C6-C10 aryl, aralkyl, or C3-C10 heteroaryl; andm is 1, 2, or 3; whereinR2a and R2b are independently selected from hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, substituted and unsubstituted aryl, substituted and unsubstituted aralkyl, hydroxy, C1-C6 alkoxy, aryloxy, aralkoxy, alkylthio, arylthio, arylsulfonyl, arylsulfinyl, substituted and unsubstituted —O(C═O)-aryl, substituted and unsubstituted —O(C═O)-aralkyl, or substituted and unsubstituted —O(C═O)—C1-C6 alkyl; whereinR2 is selected from hydrogen, C1-C6 alkyl, or C3-C6 cycloalkyl; and |